公开(公告)号：US08765973B2

公开(公告)日：2014-07-01

申请号：US13382544

申请日：2010-07-08

申请人： Douglas E. Raines ,  Joseph F. Cotten ,  Stuart A. Forman ,  Keith W. Miller ,  Syed S. Husain ,  Gregory D. Cuny

发明人： Douglas E. Raines ,  Joseph F. Cotten ,  Stuart A. Forman ,  Keith W. Miller ,  Syed S. Husain ,  Gregory D. Cuny

IPC分类号： C07D207/337 ,  A61K31/40

CPC分类号： C07D207/34 ,  A61K31/40

摘要： The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; R4 and R5 are independently H, halogen, CN or CF3; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

摘要翻译： 本发明涉及式（I）化合物：其中R1是L1C（O）OT或L1C（O）OL2C（O）OT; R2是取代或未取代的C1-C10烷基，C2-C10烯基或C2-C10炔基，或R1; n为0〜5的整数， 每个R 3独立地是卤素或R 2; R4和R5独立地为H，卤素，CN或CF3; L1和L2各自独立地为键，取代或未取代的C1-C10亚烷基，C2-C10亚烯基或C2-C10亚炔基; 和T是H，取代或未取代的C 1 -C 10烷基，C 2 -C 10烯基或C 2 -C 10炔基，硝基苯酚或环丙基。 本发明还涉及包含根据式（I）的化合物和药学上可接受的载体的药物组合物，以及通过施用这种药物组合物在哺乳动物中提供麻醉的方法。

公开(公告)号：US20130079381A1

公开(公告)日：2013-03-28

申请号：US13382544

申请日：2010-07-08

申请人： Douglas E. Raines ,  Joseph F. Cotten ,  Stuart A. Forman ,  Keith W. Miller ,  Syed S. Husain ,  Gregory D. Cuny

发明人： Douglas E. Raines ,  Joseph F. Cotten ,  Stuart A. Forman ,  Keith W. Miller ,  Syed S. Husain ,  Gregory D. Cuny

IPC分类号： C07D207/34

CPC分类号： C07D207/34 ,  A61K31/40

摘要： The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; R4 and R5 are independently H, halogen, CN or CF3; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

公开(公告)号：US20120101096A1

公开(公告)日：2012-04-26

申请号：US13257418

申请日：2010-03-22

申请人： Lizbeth K. Hedstrom ,  Gregory D. Cuny ,  Deviprasad R. Gollapalli ,  Sivapriya Kirubakaran ,  Sushil Kumar Maurya ,  Boris Striepen ,  Suresh Kumar Gorla ,  Corey Robert Johnson ,  Mandapati Kavitha ,  Jihan Khan

发明人： Lizbeth K. Hedstrom ,  Gregory D. Cuny ,  Deviprasad R. Gollapalli ,  Sivapriya Kirubakaran ,  Sushil Kumar Maurya ,  Boris Striepen ,  Suresh Kumar Gorla ,  Corey Robert Johnson ,  Mandapati Kavitha ,  Jihan Khan

IPC分类号： A61K31/535

CPC分类号： C07D401/12 ,  C07C233/15 ,  C07C235/24 ,  C07C235/38 ,  C07C237/20 ,  C07C255/60 ,  C07C275/28 ,  C07C275/30 ,  C07C275/42 ,  C07C309/15 ,  C07D209/08 ,  C07D209/12 ,  C07D209/30 ,  C07D215/38 ,  C07D235/26 ,  C07D237/32 ,  C07D249/06 ,  C07D263/56 ,  C07D263/57 ,  C07D295/192 ,  C07D401/04 ,  C07D401/14 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/08 ,  C07D491/052

摘要： Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.

摘要翻译： 本文描述了可用作IMPDH抑制剂的化合物及其药学上可接受的盐和前药。 在某些实施方案中，本发明的化合物选择性地抑制寄生IMPDH相对于宿主IMPDH。 此外，本发明提供包含一种或多种本发明化合物的药物组合物。 本发明还涉及治疗哺乳动物中各种寄生虫和细菌感染的方法。 此外，化合物可以单独使用或与其它治疗或预防剂如抗病毒剂，抗炎剂，抗微生物剂和免疫抑制剂组合使用。

公开(公告)号：US20100183658A1

公开(公告)日：2010-07-22

申请号：US12593659

申请日：2008-03-28

申请人： Kai W. Wucherpfennig ,  Melissa Joy Call ,  Xuechao Xing ,  Ross L. Stein ,  Gregory D. Cuny

发明人： Kai W. Wucherpfennig ,  Melissa Joy Call ,  Xuechao Xing ,  Ross L. Stein ,  Gregory D. Cuny

IPC分类号： A61K39/385 ,  A61K31/41 ,  A61K31/47 ,  A61K31/4439 ,  A61K31/433 ,  A61K31/427 ,  A61K31/506 ,  A61K31/497 ,  A61K31/405 ,  A61K38/02 ,  A61P37/06

CPC分类号： A61K31/405 ,  C07D209/42 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D417/12 ,  Y02A50/387 ,  Y02A50/463 ,  Y02A50/465 ,  Y02A50/471 ,  Y02A50/483

摘要： The invention provides classes of novel compounds that accelerate peptide loading to DR in the absence of DM and related pharmaceutical compositions. The invention also provides conjugates of these compounds with peptides, antigens or other MHC-based therapeutics, including peptides that self-catalyze their loading onto MHC Class II molecules. Methods are provided for modulating an immune response in a subject. Also disclosed are methods of using the novel compounds, e.g., in combination with MHC-based therapeutics, for the treatment of autoimmune diseases and for the manufacture of medicaments. Methods of improving loading of viral peptides and tumor peptides for enhancing the CD4 T cell response following vaccination against viruses or tumors, and related vaccines, are also provided.

摘要翻译： 本发明提供了在不存在DM和相关药物组合物的情况下加速肽向DR加载的新类化合物。 本发明还提供了这些化合物与肽，抗原或其他基于MHC的治疗剂的缀合物，包括自身催化其在MHC II类分子上的载体的肽。 提供用于调节受试者的免疫应答的方法。 还公开了使用新化合物的方法，例如与基于MHC的治疗剂组合用于治疗自身免疫性疾病和用于制备药物。 还提供了改善病毒肽和肿瘤肽负荷以增强针对病毒或肿瘤疫苗接种后的CD4T细胞应答的方法以及相关疫苗。

公开(公告)号：US20100143404A1

公开(公告)日：2010-06-10

申请号：US10585216

申请日：2004-12-29

申请人： Li-An Yeh ,  Gregory D. Cuny ,  Melissa Call ,  Kai Wucherpfennig ,  Ross L. Stein

发明人： Li-An Yeh ,  Gregory D. Cuny ,  Melissa Call ,  Kai Wucherpfennig ,  Ross L. Stein

IPC分类号： A61K31/381 ,  A61K39/12 ,  A61K39/02 ,  A61K39/00 ,  C07D333/40 ,  C12N5/00 ,  G01N33/53 ,  A61P37/02

CPC分类号： G01N33/5011 ,  C07D333/40 ,  G01N33/5008 ,  G01N33/502 ,  G01N33/5047 ,  G01N33/6863 ,  G01N2500/10

摘要： Compounds of formula (I), compositions, methods and kits are provided. The compounds and compositions may be particularly useful for modulating immunological responses. Formula (I) wherein, R1 is alkyl, aryl, or heterocyclyl; R2 is H, alkyl, aryl, heterocyclyl, OR3 or N(R3)2, R3 is H, alkyl, aryl, or heterocyclyl; R4 is H, CN, halogen, CF3, CO2R3, or C(O)N(R3)2; X is S, SO2, O, or NR3; and Y is S, O, or NR3.

摘要翻译： 提供式（I）化合物，组合物，方法和试剂盒。 化合物和组合物可特别用于调节免疫应答。 式（I）其中，R 1是烷基，芳基或杂环基; R2是H，烷基，芳基，杂环基，OR3或N（R3）2，R3是H，烷基，芳基或杂环基; R4是H，CN，卤素，CF3，CO2R3或C（O）N（R3）2; X是S，SO 2，O或NR 3; Y是S，O或NR 3。

公开(公告)号：US07517892B2

公开(公告)日：2009-04-14

申请号：US09951130

申请日：2001-09-12

申请人： Brian M. Aquila ,  Thomas D. Bannister ,  Gregory D. Cuny ,  James R. Hauske ,  Joanne M. Holland ,  Paul E. Persons ,  Heike Radeke ,  Fengjiang Wang ,  Liming Shao

发明人： Brian M. Aquila ,  Thomas D. Bannister ,  Gregory D. Cuny ,  James R. Hauske ,  Joanne M. Holland ,  Paul E. Persons ,  Heike Radeke ,  Fengjiang Wang ,  Liming Shao

IPC分类号： A61P25/00 ,  A61K31/445 ,  C07D211/00 ,  C07D401/00

CPC分类号： C40B40/04 ,  C07B2200/11 ,  C07C255/46 ,  C07C2601/04 ,  C07D205/02 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D211/12 ,  C07D211/16 ,  C07D211/18 ,  C07D211/20 ,  C07D211/26 ,  C07D211/32 ,  C07D211/40 ,  C07D211/42 ,  C07D211/60 ,  C07D233/04 ,  C07D233/10 ,  C07D265/30 ,  C07D267/10 ,  C07D303/08 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C40B30/04 ,  C40B50/14

摘要： One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

摘要翻译： 本发明的一个方面涉及杂环化合物。 本发明的第二方面涉及杂环化合物作为各种哺乳动物细胞受体（包括多巴胺，5-羟色胺或去甲肾上腺素转运蛋白）的配体的用途。 本发明的化合物可用于治疗多种疾病，疾病，其包括但不限于成瘾，焦虑，抑郁，性功能障碍，高血压，偏头痛，阿尔茨海默病，肥胖，呕吐，精神病， 精神分裂症，帕金森病，炎症性疼痛，神经性疼痛，Lesche-Nyhane病，Wilson氏病和Tourette综合征。 本发明的另一方面涉及杂环化合物的组合文库的合成，以及用于生物活性的那些文库的筛选，例如在基于多巴胺转运蛋白的测定中。

公开(公告)号：US06645980B1

公开(公告)日：2003-11-11

申请号：US09717174

申请日：2000-11-20

申请人： Gregory D. Cuny ,  Liming Shao ,  James R. Hauske ,  Michele L. R. Heffernan ,  Brian M. Aquila ,  Xinhe Wu ,  Fengjiang Wang ,  Thomas D. Bannister

发明人： Gregory D. Cuny ,  Liming Shao ,  James R. Hauske ,  Michele L. R. Heffernan ,  Brian M. Aquila ,  Xinhe Wu ,  Fengjiang Wang ,  Thomas D. Bannister

IPC分类号： A61K31445

CPC分类号： C07D265/30 ,  A61K31/397 ,  A61K31/438 ,  A61K31/4523 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/551 ,  A61K31/553 ,  C07D205/04 ,  C07D211/26 ,  C07D211/56 ,  C07D211/60 ,  C07D211/70 ,  C07D223/04 ,  C07D223/10 ,  C07D241/04 ,  C07D243/08 ,  C07D267/10 ,  C07D333/38 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/06

摘要： One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

公开(公告)号：US06635661B2

公开(公告)日：2003-10-21

申请号：US09798803

申请日：2001-03-02

申请人： Gregory D. Cuny ,  Liming Shao ,  James R. Hauske ,  Michele L. R. Heffernan ,  Brian M. Aquila ,  Xinhe Wu ,  Fengjiang Wang ,  Thomas D. Bannister

发明人： Gregory D. Cuny ,  Liming Shao ,  James R. Hauske ,  Michele L. R. Heffernan ,  Brian M. Aquila ,  Xinhe Wu ,  Fengjiang Wang ,  Thomas D. Bannister

IPC分类号： A61K31445

CPC分类号： C07D221/04 ,  A61K31/397 ,  A61K31/438 ,  A61K31/4523 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/551 ,  A61K31/553 ,  C07D205/04 ,  C07D205/06 ,  C07D211/26 ,  C07D211/42 ,  C07D211/56 ,  C07D211/60 ,  C07D211/70 ,  C07D223/04 ,  C07D223/10 ,  C07D241/04 ,  C07D243/08 ,  C07D265/30 ,  C07D267/10 ,  C07D333/38 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D491/10

摘要： One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

公开(公告)号：USRE38251E1

公开(公告)日：2003-09-16

申请号：US09512423

申请日：2000-02-23

申请人： Stanley C. Busman ,  Richard J. Ellis ,  Jeanne E. Haubrich ,  William D. Ramsden ,  Tran Van Thien ,  Gregory D. Cuny

发明人： Stanley C. Busman ,  Richard J. Ellis ,  Jeanne E. Haubrich ,  William D. Ramsden ,  Tran Van Thien ,  Gregory D. Cuny

IPC分类号： G03F7021

CPC分类号： G03F7/0045 ,  C09B57/007 ,  G03F7/0382 ,  G03F7/0392 ,  Y10S430/121 ,  Y10S430/127 ,  Y10S430/145 ,  Y10S430/146

摘要： Photochemical acid progenitors in combination with dihydroperimidine squarylium dyes have been found to be particularly effective at generating acid upon irradiation with new-infrared radiation. It has been found that dihydroperimidine squarylium dyes that are particularly useful in this invention have an oxidation potential greater than about 0.5 V relative to SCE as measured in dichloromethane.

公开(公告)号：US5723617A

公开(公告)日：1998-03-03

申请号：US576502

申请日：1995-12-21

申请人： Gregory D. Cuny

发明人： Gregory D. Cuny

IPC分类号： C07D471/04 ,  C09B23/00 ,  C09B57/00 ,  C09K3/00 ,  G03C1/498 ,  G03C1/83 ,  G03C5/16 ,  G11B7/244 ,  G11B7/247 ,  C07D221/06

CPC分类号： C07D471/04 ,  C09B57/00 ,  G03C1/4989 ,  G03C1/832 ,  G03C5/164 ,  G11B7/244 ,  G11B7/247 ,  G03C1/83

摘要： A series of novel pyrrolo�2,1-a!isoquinoline dyes has been prepared using readily available starting materials via a simple synthetic pathway. These dyes have narrow absorption bands in the range of 500-900 nm. Those that absorb in the near-infrared region (700-1400 nm) lack significant absorption in the 300-400 nm ultraviolet region of the spectrum; this is an advantage for use in an applications such as imaging setting film. In addition, the greater thermal and chemical stability of these dyes in comparison to their indolizine analogues should be valuable in many applications.

摘要翻译： 已经使用容易获得的原料通过简单的合成途径制备了一系列新的吡咯并[2,1-a]异喹啉染料。 这些染料在500-900nm的范围内具有窄的吸收带。 在近红外区域（700-1400nm）吸收的那些在光谱的300-400nm紫外区域中没有显着的吸收; 这是用于诸如成像设置膜的应用中的优点。 此外，与其中和衍生物类似物相比，这些染料的更高的热和化学稳定性在许多应用中应当是有价值的。